BOLD-100 NKP-1339; IT-139; KP-1339|cas:197723-00-5|西域试剂

BOLD-100 NKP-1339; IT-139; KP-1339,98.14%

产品编号：Bellancom-16350| CAS NO：197723-00-5| 分子式：C₁₄H₁₂Cl₄N₄NaRu| 分子量：502.14

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货号	价格	库存与货期
Bellancom-16350	￥3500.00	杭州北京（现货）
Bellancom-16350	￥5000.00	杭州北京（现货）
Bellancom-16350	￥15000.00	杭州北京（现货）
Bellancom-16350	￥21000.00	杭州北京（现货）

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BOLD-100 NKP-1339; IT-139; KP-1339

产品介绍

BOLD-100 (NKP-1339; IT-139) 是针对实体癌开发的一流钌抗癌试剂，副作用小。BOLD-100 通过线粒体途径诱导 G2/M 细胞周期停滞，DNA 合成阻断 (DNA synthesis) 和诱导细胞凋亡 (apoptosis)。BOLD-100 具有很高的肿瘤靶向潜力，与血清蛋白 (serum proteins) 如白蛋白和转铁蛋白强烈结合，并在还原性肿瘤环境中激活。

生物活性

BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu.

体外研究

BOLD-100 (0-200 μM; 72 hours) has the anticancer activity against malignant cell lines of diverse origin, exhibits IC₅₀ values of 45-200?μM for KP1339 mono-therapy. It against Hepatoma cell line, Hep3B, HepG2, PLC/PRF/5 and HCC2 cells with the Mean IC₅₀ value of 186.3 μM, 165.4 μM, 124.4 μM, and 69.4 μM, respectively. It against Melanoma cell line, VM-1, VM-21,VM-48 with IC₅₀ values of 178 μM, 111 μM, and 143 μM, respectively. It against Lung cancer and Colon cancer cell lines, inhibits A549, VL-8, SW480 and HCT116 cells, respectively.
BOLD-100 (0-150 μM; 24 hours) induces cell apoptosis alone. When it combines with sorafenib, it increases the numbers of the apopotic cells. Additionally, the p-PARP and caspase 7 cleavage is promoted either.
BOLD-100 (0-150 μM; 24 hours) can promote phosphorylation of STAT3 and CREB expression, however, the decreasation is inhibited by sorafenib cotreatment.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	Hepatoma, Melanoma, Lung cancer and Colon cancer cell lines
Concentration:	0 μM, 50 μM, 100 μM, 150 μM and 200 μM
Incubation Time:	72 hours
Result:	Has anti-cancer activity in diverse malignant tumour cell types.

Apoptosis Analysis

Cell Line:	Hep3B cells
Concentration:	0 μM, 75 μM, 150 μM
Incubation Time:	72 hours
Result:	Promoted cell apoptosis as a concentration manner.

Western Blot Analysis

Cell Line:	Hep3B cells
Concentration:	0 μM, 75 μM, 150 μM
Incubation Time:	72 hours
Result:	Increased p-STAT3 and p-CREB expression in cells without sorafenib cotreatment.

体内研究
(In Vivo)

BOLD-100 (intravenous injection; 30 mg/kg; once a week; 42sdays) combines with the multi-kinase inhibitor sorafenib and exhibits a further anticancer activity when compares to the BOLD-100 treatment alone in Hep3B xenografts grown in Balb/c SCID mice .

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Hep3B xenograft in Balb/c mice
Dosage:	30 mg/kg
Administration:	Intravenous injection
Result:	Had synergistic activity of KP1339 with sorafenib in vivo.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Hep3B xenograft in Balb/c mice
Dosage:	30 mg/kg
Administration:	Intravenous injection
Result:	Had synergistic activity of KP1339 with sorafenib in vivo.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Hep3B xenograft in Balb/c mice
Dosage:	30 mg/kg
Administration:	Intravenous injection
Result:	Had synergistic activity of KP1339 with sorafenib in vivo.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 59 mg/mL (117.50 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9915 mL	9.9574 mL	19.9148 mL
5 mM	0.3983 mL	1.9915 mL	3.9830 mL
10 mM	0.1991 mL	0.9957 mL	1.9915 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献